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324842 | EGFR/ErbB-2/ErbB-4 Inhibitor II - CAS 944341-54-2 - Calbiochem

324842
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₂₇ClN₆O₃ • HCl 944341-54-2

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      324842-5MG
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      Stocked 
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable aminopyrimidine oxime compound that potently inhibits EGFR/ErbB1/HER1, ErbB2/HER2/neu, and ErbB4/HER4 kinase activity (IC50 = 22, 38 and 21 nM, respectively) in an ATP-competitive manner and effectively suppresses cellular receptor phosphorylation (IC50 = 223 and 107 nM against basal HER2 and EGF-induced EFGR phosphorylation, respectively, in SKBR3 and A431 cultures) as well as HER2- and EGFR-dependent cancer cell proliferations (IC50 <1µM), while exhibiting much reduced or little activity against a panel of 202 other kniases. Reported to be orally available and blood-brain barrier permeant in both mice and rats and be efficacious in inhibiting tumor growth in several murine xenograft models (100 to 200 mg/kg/day, p.o.) in vivo.
          Catalogue Number324842
          Brand Family Calbiochem®
          Synonyms(E)-4-Amino-6-(4-benzyloxy-3-chloro-phenylamino)-pyrimidine-5-carbaldehyde-O-(2-morpholin-4-yl-ethyl)-oxime, HCl, JNJ-28871063, HCl
          Application Data
          References
          ReferencesEmanuel, S.L., et al. 2008. Mol. Pharmacol. 73, 338.
          Product Information
          CAS number944341-54-2
          FormBeige solid
          Hill FormulaC₂₄H₂₇ClN₆O₃ • HCl
          Chemical formulaC₂₄H₂₇ClN₆O₃ • HCl
          Hygroscopic Hygroscopic
          Applications
          Biological Information
          Purity≥95% by HPLC
          Physicochemical Information
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          Storage -20°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          324842

          References

          Reference overview
          Emanuel, S.L., et al. 2008. Mol. Pharmacol. 73, 338.
          Data Sheet

          Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

          Revision06-August-2010 RFH
          Synonyms(E)-4-Amino-6-(4-benzyloxy-3-chloro-phenylamino)-pyrimidine-5-carbaldehyde-O-(2-morpholin-4-yl-ethyl)-oxime, HCl, JNJ-28871063, HCl
          Application Data
          DescriptionA cell-permeable aminopyrimidine oxime compound that potently inhibits EGFR/ErbB1/HER1, ErbB2/HER2/neu, and ErbB4/HER4 kinase activity (IC50 = 22, 38 and 21 nM, respectively) in an ATP-competitive manner and effectively suppresses cellular receptor phosphorylation (IC50 = 223 and 107 nM against basal HER2 and EGF-induced EFGR phosphorylation, respectively, in SKBR3 and A431 cultures) as well as HER2- and EGFR-dependent cancer cell proliferations (IC50 <1µM), while exhibiting much reduced or little activity against a panel of 202 other kniases. Reported to be orally available and blood-brain barrier permeant in both mice and rats and be efficacious in inhibiting tumor growth in several murine xenograft models (100 to 200 mg/kg/day, p.o.) in vivo.
          FormBeige solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number944341-54-2
          Chemical formulaC₂₄H₂₇ClN₆O₃ • HCl
          Purity≥95% by HPLC
          SolubilityDMSO (25 mg/ml)
          Storage -20°C
          Protect from light
          Hygroscopic
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesEmanuel, S.L., et al. 2008. Mol. Pharmacol. 73, 338.